Assay Detail
Binding
CHEMBL4432075
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Binding affinity to human recombinant DPP4 (39 to 766 residues) at 5 uM by isothermal titration calorimetry
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 9 | 7.75 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL237500 | LINAGLIPTIN | 4.0 | 1 | 8.28 |
| CHEMBL237067 | — | — | 1 | 8.04 |
| CHEMBL142703 | VILDAGLIPTIN | 4.0 | 1 | 7.97 |
| CHEMBL2147777 | TENELIGLIPTIN | 4.0 | 1 | 7.92 |
| CHEMBL1422 | SITAGLIPTIN | 4.0 | 1 | 7.87 |
| CHEMBL385517 | SAXAGLIPTIN ANHYDROUS | 4.0 | 1 | 7.80 |
| CHEMBL399216 | — | — | 1 | 7.73 |
| CHEMBL376359 | ALOGLIPTIN | 4.0 | 1 | 7.54 |
| CHEMBL4456228 | — | — | 1 | 6.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL237500 | LINAGLIPTIN | Kd | = | 5.3 | nM | 8.28 |
| CHEMBL237067 | — | Kd | = | 9.2 | nM | 8.04 |
| CHEMBL142703 | VILDAGLIPTIN | Kd | = | 10.7 | nM | 7.97 |
| CHEMBL2147777 | TENELIGLIPTIN | Kd | = | 11.9 | nM | 7.92 |
| CHEMBL1422 | SITAGLIPTIN | Kd | = | 13.5 | nM | 7.87 |
| CHEMBL385517 | SAXAGLIPTIN ANHYDROUS | Kd | = | 15.9 | nM | 7.80 |
| CHEMBL399216 | — | Kd | = | 18.6 | nM | 7.73 |
| CHEMBL376359 | ALOGLIPTIN | Kd | = | 28.5 | nM | 7.54 |
| CHEMBL4456228 | — | Kd | = | 246.0 | nM | 6.61 |